Radiolabeled enzyme inhibitors and binding agents targeting PSMA: Effective theranostic tools for imaging and therapy of prostate cancer

Nuclear Medicine and Biology

Volumn 43, Issue 11, 2016, Pages 692-720

  Pillai, Maroor Raghavan Ambikalmajan ^a   Nanabala, Raviteja ^b   Joy, Ajith ^a   Sasikumar, Arun ^b   Russ Knapp, Furn F ^c  

^a Molecular Group of Companies   (India)

^b KIMS Hospital   (India)

^c OAK RIDGE NATIONAL LABORATORY   (United States)

Author keywords

Enzyme inhibitors; Gallium 68; Lutetium 177; Prostate cancer; Prostate specific membrane antigen; Targeted radionuclide therapy

Indexed keywords

2 PHOSPHONOMETHYL PENTANEDIOIC ACID; 2 [3 [1 CARBOXY 5 (4 IODOBENZOYLAMINO)PENTYL]UREIDO]PENTANEDIOIC ACID I 125; 2 [3 [1 CARBOXY 5 [(6 FLUOROPYRIDINE 2 CARBONYL)AMINO]PENTYL]UREIDO]PENTANEDOIC ACID F 18; 4,4' PHOSPHINICOBIS(BUTANE 1,3 DICARBOXYLIC ACID); CARBON N [N [(1,3 DICARBOXYPROPYL)CARBOMOYL]METHYL LEVO CYSTEINE] C 11; CHEMICAL COMPOUND; GALLIUM 68; GALLIUM PROSTATE SPECIFIC MEMBRANE ANTIGEN 11 GA 68; HYDROXAMIC ACID DERIVATIVE; IODINE 124; IODINE 131; IODINE MIP1095 I 131; LUTETIUM 177; LUTETIUM PROSTATE SPECIFIC MEMBRANE ANTIGEN 617 LU 177; LUTETIUM PROSTATE SPECIFIC MEMBRANE ANTIGEN EUK SUB KFF [1,4,7,10 TETRAAZACYCLDODECANE 1(GLUTARIC ACID) 4,7,10 TRIACETIC ACID]PROSTATE SPECIFIC MEMBTANE ANTIGEN TUM 1 LU177; MONOCLONAL ANTIBODY; N ACETYL LEVO ASPARTYL LEVO GLUTAMATE; N N SUCCINIMIDYL 4 FLUOROBENZOATE F 18; N[N (1,3 DICARBOXYPROPYL)CARBAMOYL] 4 FLUOROBENZYL LEVO CYSTEINE F 18; PROSTATE SPECIFIC ANTIGEN; PROSTATE SPECIFIC MEMBRANE ANTIGEN; RADIOISOTOPE; RADIOPHARMACEUTICAL AGENT; SULFONAMIDE; THIOL DERIVATIVE; TROFOLASTAT TC 99M; TUMOR MARKER; UNCLASSIFIED DRUG; ENZYME INHIBITOR; GLUTAMATE CARBOXYPEPTIDASE II; GLUTAMATE CARBOXYPEPTIDASE II, HUMAN; MEMBRANE ANTIGEN;

BINDING SITE; CANCER DIAGNOSIS; CANCER RADIOTHERAPY; CANCER THERAPY; CASTRATION RESISTANT PROSTATE CANCER; CHEMICAL STRUCTURE; DRUG STRUCTURE; ENZYME ACTIVITY; ENZYME BINDING; HUMAN; IMAGING; INTESTINE ADENOCARCINOMA; INTESTINE CANCER; ISOTOPE LABELING; KIDNEY CARCINOMA; METASTASIS; NONHUMAN; PHARMACOPHORE; POSITRON EMISSION TOMOGRAPHY; PROSTATE CANCER; PROSTATE METASTASIS; PROTEIN EXPRESSION; RADIATION ABSORPTION; RADIOACTIVITY; REVIEW; SINGLE PHOTON EMISSION COMPUTER TOMOGRAPHY; STRUCTURE ACTIVITY RELATION; THYROID PAPILLARY CARCINOMA; ANTAGONISTS AND INHIBITORS; DIAGNOSTIC IMAGING; MALE; METABOLISM; MOLECULARLY TARGETED THERAPY; PATHOLOGY; PROCEDURES; PROSTATIC NEOPLASMS;

ANTIGENS, SURFACE; DIAGNOSTIC IMAGING; ENZYME INHIBITORS; GLUTAMATE CARBOXYPEPTIDASE II; HUMANS; MALE; MOLECULAR TARGETED THERAPY; PROSTATIC NEOPLASMS;

EID: 84989879871     PISSN: 09698051     EISSN: 18729614     Source Type: Journal    
DOI: 10.1016/j.nucmedbio.2016.08.006     Document Type: Review

References (248)

1. [1] World Cancer Research Foundation, http://www.wcrf.org/int/cancer-facts-figures/worldwide-data [Accessed on 30.3.2015].
2. [2] American Cancer Society, Key statistics for prostate cancer. http://www.cancer.org/cancer/prostatecancer/detailedguide/prostate-cancer-key-statistics [Accessed on 30.3.2015].
3. [3] Guidelines for the management of clinically localized prostate cancer. https://www.auanet.org/education/guidelines/prostate-cancer.cfm, 2007 [Accessed on 30.3.2015].
4. [4] Bouchelouche, K, Tagawa, ST, Goldsmith, SJ, Turkbey, B, Capala, J, Choyke, P, PET/CT imaging and radioimmunotherapy of prostate cancer. Semin Nucl Med 41 (2011), 29–44.
5. [5] Jadvar, H, Molecular imaging of prostate cancer: PET radiotracers. AJR Am J Roentgenol 199 (2012), 278–291.
6. [6] Aparici, CM, Seo, Y, Functional imaging for prostate cancer: therapeutic implications. Semin Nucl Med 42 (2012), 328–342.
7. [7] Bouchelouche, K, Turkbey, B, Choyke, P, Capala, J, Imaging prostate cancer: an update on positron emission tomography and magnetic resonance imaging. Curr Urol Rep 11 (2010), 180–190.
8. [8] Kiess, AP, Cho, SY, Pomper, MG, Translational molecular imaging of prostate cancer. Curr Radiol Rep 1 (2013), 216–226.
9. 11C-choline PET/CT. Nucl Med 40 (2015), 386–391.
10. 68Ga]gallium labeled PSMA ligand for the diagnosis of prostate cancer: biodistribution in humans and first evaluation in tumor lesions. Eur J Nucl Med Mol Imaging 40 (2013), 486–495.
11. 177Lu-DKFZ-617 PSMA of castrate-resistant metastatic prostate cancer: a two-centre study. Eur J Nucl Med Mol Imaging Res, 5, 2015, 36.
12. [12] Baum, RP, Kulkarni, HR, Schuchardt, C, Singh, A, Wirtz, M, Wiessalla, S, et al. Lutetium-177 PSMA radioligand therapy of metastatic castration-resistant prostate cancer: safety and efficacy. J Nucl Med, 2016 [Epub ahead of print].
13. [13] Weissleder, R, Molecular imaging in cancer. Science 312 (2006), 1168–1171.
14. [14] Pysz, MA, Gambhir, SS, Willmann, JK, Molecular imaging: current status and emerging strategies. Clin Radiol 65 (2010), 500–516.
15. [15] Kirsher, MF, Hricak, H, Larson, SM, Molecular imaging for personalized cancer care. Mol Oncol 6 (2012), 182–195.
16. [16] Weibo Cai, W, Chen, X, Multimodality molecular imaging of tumor angiogenesis. J Nucl Med 49 (2008), 113S–128S.
17. [17] Buck, A.K., Reske, S.N., Cellular origin and molecular mechanisms of 18F-FDG uptake: is there a contribution of the endothelium?. J Nucl Med 45 (2004), 461–463.
18. [18] Goldenberg, D.M., (eds.) Cancer imaging with radiolabeled antibodies, 1990, Springer. Kluver Academic Publications [ https://books.google.co.in/books?isbn=1461314976].
19. [19] Eckelman, WC, Reba, RC, Gibson, RE, Rzeszotarski, WJ, Vieras, F, Mazaitis, JK, et al. Receptor-binding radiotracers: a class of potential radiopharmaceuticals. J Nucl Med 20 (1979), 350–357.
20. [20] Wangler, C, Buchmann, I, Eisenhut, M, Haberkorn, U, Mier, W, Radiolabeled peptides and proteins in cancer therapy. Protein Pept Lett 143 (2007), 273–279.
21. 177Lu-DOTA-TATE for PRRT. Curr Radiopharm 9 (2016), 8–18.
22. [22] Carollo, A, Papi, S, Chinol, M, Lutetium-177 labelled peptides: the European Institute of Oncology experience. Curr Radiopharm 9 (2016), 19–32.
23. [23] Zhou, J, Neale, JH, Pomper, MG, Kozikowski, AP, NAAG peptidase inhibitors and their potential potency for diagnosis and therapy. Nat Rev Drug Discov 4 (2005), 1015–1026.
24. [24] Dash, A, Pillai, MRA, Knapp, FF Jr., Targeted radionuclide therapy. Curr Radiopharm 6 (2013), 152–180.
25. [25] Dash, A, Chakraborthy, S, Pillai, MRA, Knapp, FF, Peptide receptor radionuclide therapy: an overview. Cancer Biother Radiopharm 30 (2015), 47–71.
26. [26] Srinivas, PR, Kramer, BS, Srivastava, S, Trends in biomarker research for cancer detection. Lancet Oncol 2 (2001), 698–704.
27. [27] Bhatt, AN, Mathur, R, Farooque, A, Verma, A, Dwarakanath, BS, Cancer biomarkers — current perspectives. Ind J Med Res 132 (2010), 129–149.
28. [28] Bigbee, W, Herberman, RB, Tumor markers and immunodiagnosis. Bast, R.C. Jr., Kufe, D.W., Pollock, R.E., et al. (eds.) Cancer medicine, 6th ed., 2003, BC Decker Inc., Hamilton, Ontario, Canada.
29. [29] National Cancer Institute, Tumor markers. http://www.cancer.gov/about-cancer/diagnosis-staging/diagnosis/tumor-markers-fact-sheet [Accessed on 31.03.2016].
30. [30] Farinati, F, Marino, D, De Giorgio, M, Baldan, A, Cantarini, M, Cursaro, C, et al. Diagnostic and prognostic role of α-fetoprotein in hepatocellular carcinoma: both or neither?. Am J Gastroenterol 101 (2006), 524–532.
31. [31] Ballehaninna, UK, Chamberlain, RS, Biomarkers for pancreatic cancer: promising new markers and options beyond CA 19-9. Tumour Biol 34 (2013), 3279–3292.
32. [32] Bast, RC Jr., Urban, N, Shridhar, V, Smith, D, Zhang, Z, Skates, S, et al. Early detection of ovarian cancer: promise and reality. Cancer Treat Res 107 (2002), 61–97.
33. [33] Henze, G, Dummer, R, Joller-Jemelka, HI, Böni, R, Burg, G, Serum S100 — a marker for disease monitoring in metastatic melanoma. Dermatology 194 (1997), 208–212.
34. [34] Clarke, RA, Schirra, HJ, Catto, JW, Lavin, MF, Gardiner, RA, Markers for detection of prostate cancer. Cancers 2 (2010), 1125–1154.
35. [35] Madu, CO, Lu J, Y, Novel diagnostic biomarkers for prostate cancer. J Cancer 1 (2010), 150–177.
36. [36] Papsidero, LD, Wang, MC, Valenzuela, LA, Murphy, GP, Chu, TMA, Prostate antigen in sera of prostatic cancer patients. Cancer Res 40 (1980), 2428–2432.
37. [37] Denmeade, SR, Isaacs, JT, The role of prostate-specific antigen in the clinical evaluation of prostatic disease. BJU Int 93 (2004), 10–15.
38. [38] Schröder, FH, Hugosson, J, Roobol, MJ, Tammela, TL, Ciatto, S, Nelen, V, et al. Screening and prostate-cancer mortality in a randomized European study. N Engl J Med 360 (2009), 1320–1328.
39. [39] American Cancer Society, What tests can detect prostate cancer early?. http://www.cancer.org/cancer/prostatecancer/moreinformation/prostatecancerearlydetection/prostate-cancer-early-detection-tests [Accessed on 31.03.2016].
40. [40] Etzioni, R, Penson, DF, Legler, JM, di Tommaso, D, Boer, R, Gann, PH, et al. Over-diagnosis due to prostate-specific antigen screening: lessons from U.S. prostate cancer incidence trends. J Natl Cancer Inst 94 (2002), 981–990.
41. [41] Silver, DA, Pellicer, J, Fair, WR, Heston, WD, Cordon-Cardo, C, Prostate-specific membrane antigen expression in normal and malignant human tissues. Clin Cancer Res 3 (1997), 81–85.
42. [42] Murphy, GP, Elgamal, AA, Su, SL, Bostwick, DG, Holmes, EH, Current evaluation of the tissue localization and diagnostic utility of prostate specific membrane antigen. Cancer 83 (1998), 2259–2269.
43. [43] Osborn, JR, Akhtar, NH, Vallabhajosula, S, Anand, A, Deh, K, Tagawa, ST, Prostate specific membrane-based imaging. Urol Oncol 31 (2013), 144–154.
44. [44] Deras, IL, Aubin, SM, Blase, A, Day, JR, Koo, S, Partin, AW, et al. PCA3: a molecular urine assay for predicting prostate biopsy outcome. J Urol 179 (2008), 1587–1592.
45. [45] Mhawech-Fauceglia, Smiraglia, DJ, Hashara, W, Andrews, C, Schwaller, J, South, S, et al. Prostate-specific membrane antigen expression is a potential prognostic marker in endometrial adenocarcinoma. Cancer Epidemiol Biomarkers Rev 17 (2008), 571–577.
46. [46] Chang, SS, O'Keefe, DS, Bacich, DJ, Reuter, VE, Heston, WD, Gaudin, PB, Prostate-specific membrane antigen is produced in tumor-associated neovasculature. Clin Cancer Res 5 (1999), 2674–2681.
47. [47] Chang, SS, Reuter, VE, Heston, WD, Bander, NH, Grauer, LS, Gaudin, PB, Five different prostate membrane antigen (PSMA) antibodies confirm PSMA expression in tumor-associated neovasculature. Cancer Res 59 (1999), 3192–3198.
48. [48] Haffner, MC, Kronberger, IE, Ross, JS, Sheehan, CE, Zitt, M, Mühlmann, G, et al. Prostate-specific membrane antigen expression in the neovasculature of gastric and colorectal cancers. Hum Pathol 40 (2009), 1754–1761.
49. [49] Haffner, MC, Lanier, J, Chaux, A, Schäfer, G, Obrist, P, Brunner, A, et al. High expression of prostate-specific membrane antigen in the tumor-associated neo-vasculature is associated with worse prognosis in squamous cell carcinoma of the oral cavity. Mod Pathol 25 (2012), 1079–1085.
50. [50] Ghosh, A, Heston, WD, Tumor target prostate specific membrane antigen (PSMA) and its regulation in prostate cancer. J Cell Biochem 91 (2004), 528–539.
51. [51] Davis, MI, Bennett, MJ, Thomas, LM, Bjorkman, PJ, Crystal structure of prostate-specific membrane antigen, a tumor marker and peptidase. Proc Natl Acad Sci U S A 102 (2005), 5981–5986.
52. [52] Rong, SB, Zhang, J, Neale, JH, Wroblewski, JT, Wang, S, Kozikowski, AP, Molecular modeling of the interactions of glutamate carboxypeptidase II with its potent NAAG-based inhibitors. J Med Chem 45 (2002), 4140–4152.
53. [53] Barinka, C, Starkova, J, Konvalinka, J, Lubkowski, J, A high resolution structure of ligand-free human glutamate carboxypeptidase. Acta Crystallogr Sect F Struct Biol Cryst Commun F63 (2007), 150–153.
54. [54] Barinka, C, Hlouchova, K, Rovenska, M, Majer, P, Dauter, M, Hin, N, et al. Structural basis of interactions between human glutamate carboxypeptidase II and its substrate analogs. J Mol Biol 376 (2008), 1438–1450.
55. [55] Chang, SS, Overview of prostate-specific membrane antigen. Rev Urol 6:Suppl. 10 (2004), S13–S18.
56. [56] Horoszewicz, JS, Leong, SS, Kawinski, E, Karr, JP, Rosenthal, H, Chu, TM, et al. LNCaP model of human prostatic carcinoma. Cancer Res 43 (1983), 1809–1818.
57. [57] Lam, JS, Yamashiro, J, Shintaku, P, Vessella, RL, Jenkins, RB, Horvath, S, et al. Prostate stem cell antigen is overexpressed in prostate cancer metastases. Clin Cancer Res 11 (2005), 2591–2596.
58. [58] Reiter, RE, Gu, Z, Watabe, T, Thomas, G, Szigeti, K, Davis, E, et al. Prostate stem cell antigen: a cell surface marker overexpressed in prostate cancer. Proc Nat Acad Sci USA 95 (1998), 1735–1740.
59. [59] Saeki, N, Gu, J, Yoshida, T, Wu, X, Prostate stem cell antigen (PSCA): a Jekyll and Hyde molecule ?. Clin Cancer Res 16 (2010), 3533–3538.
60. [60] Xu, LL, Stackhouse, BG, Florence, K, Zhang, W, Shanmugam, N, Sesterhenn, IA, et al. PSGR, a novel prostate-specific gene with homology to a G protein-coupled receptor, is overexpressed in prostate cancer. Cancer Res 60 (2000), 6568–6572.
61. [61] Xia, C, Wenbin, MW, Fen, WF, Hua, Sb, Liu, M, Identification of a prostate-specific G-protein coupled receptor in prostate cancer. Oncogene 20 (2001), 5903–5907.
62. [62] Gomes, IM, Santos, CR, Maia, CJ, Expression of STEAP1 and STEAP1B in prostate cell lines, and the putative regulation of STEAP1 by post-transcriptional and post-translational mechanisms. Genes Cancer 5 (2014), 142–151.
63. [63] Bussemakers, MJG, Bokhoven, AV, Verhaegh, GW, Smit, FP, Karthaus, HF, Schalken, JA, et al. DD3: a new prostate-specific gene, highly overexpressed in prostate cancer. Can Res 59 (1999), 5875–5979.
64. [64] Leyton, JV, Olafsen, T, Lepin, EJ, Hahm, S, Bauer, KB, Reiter, RE, et al. Humanized radioiodinated minibody for imaging of prostate stem cell antigen-expressing tumors. Clin Cancer Res 14 (2008), 7488–7496.
65. [65] Afshar-Olafsen, T, Gu, Z, Sherman, MA, Leyton, JV, Witkosky, ME, Shively, JE, et al. Targeting, imaging and therapy using a humanized antiprostate stem cell antigen (PSCA) antiboby. J Immuntother 30 (2007), 396–405.
66. [66] Yao, D, Trabulsi, EJ, Kostakoglu, L, Vallabhajosula, S, Joyce, MA, Nanus, DM, et al. The utility of monoclonal antibodies in the imaging of prostate cancer. Semin Urol Oncol 20 (2002), 211–218.
67. 11C-MCG: synthesis, uptake selectivity, and primate PET of a probe for glutamate carboxypeptidase II (NAALADase). Mol Imaging 2 (2002), 96–101.
68. [68] Pinto, JT, Suffoletto, BP, Berzin, TM, Qiao, CH, Lin, S, Tong, WP, et al. Prostate-specific membrane antigen: a novel folate hydrolase in human prostatic carcinoma cells. Clin Cancer Res 2 (1996), 1445–1451.
69. [69] Horoszewicz, JS, Kawinski, E, Murphy, GP, Monoclonal antibodies to a new antigenic marker in epithelial prostatic cells and serum of prostatic cancer patients. Anticancer Res 7 (1987), 927–935.
70. [70] Taneja, SS, ProstaScint® scan: contemporary use in clinical practice. Rev Urol 6:Suppl. 10 (2004), S19–S28.
71. [71] Kahn, D, Williams, RD, Haseman, MK, Reed, NL, Miller, SJ, Gerstbrein, J, Radioimmunoscintigraphy with In-111-labeled capromab pendetide predicts prostate cancer response to salvage radiotherapy after failed radical prostatectomy. J Clin Oncol 16 (1998), 284–289.
72. 111Indium-capromab pendetide in the evaluation of patients with residual or recurrent prostate cancer after radical prostatectomy. J Urol 159 (1998), 2041–2047.
73. [73] Sodee, DB, Malguria, N, Faulhaber, P, Resnick, MI, Albert, J, Bakale, G, et al. Multi-center ProstaScint® imaging findings in 2154 patients with prostate cancer. The ProstaScint imaging centers. Urology 56 (2000), 988–993.
74. [74] Michaels, EK, Blend, M, Quintana, JC, 111-Indium-capromab pendetide unexpectedly localizes to renal cell carcinoma. J Urol 161 (1999), 597–598.
75. [75] Zanzi, I, Stark, R, Detection of a non-Hodgkin's lymphoma by capromab pendetide scintigraphy (ProstaScint®) in a patient with prostate carcinoma. Urology, 60, 2002, 514.
76. [76] Franc, BL, Hank, LM, Detection of recurrent non-Hodgkin lymphoma on In-111 capromab pendetide imaging. Clin Nucl Med 26 (2001), 568–569.
77. [77] Zucker, RJ, Bradley, YC, Indium-111 capromab pendetide (ProstaScint) uptake in a meningioma. Clin Nucl Med 26 (2001), 568–569.
78. [78] Khan, A, Caride, VJ, Indium-111 capromab pendetide (ProstaScint) uptake in neurofibromatosis. Urology, 56, 2000, 154.
79. [79] Liu, H, Moy, P, Kim, S, Xia, Y, Rajasekaran, A, Navarro, V, et al. Monoclonal antibodies to the extracellular domain of prostate-specific membrane antigen also react with tumor vascular endothelium. Cancer Res 57 (1997), 3629–3634.
80. [80] Milowsky, MI, Nanus, DM, Kostakoglu, L, Sheehan, CE, Vallabhajosula, S, Goldsmith, SJ, et al. Vascular targeted therapy with anti-prostate-specific membrane antibody J591 in advanced solid tumors. J Clin Oncol 25 (2007), 540–547.
81. [81] Smith-Jones, PM, Vallabhajousla, S, Navarro, V, Bastidas, D, Goldsmith, SJ, Bander, NH, Radiolabeled monoclonal antibodies specific to the extracellular domain of prostate-specific membrane antigen: preclinical studies in nude mice bearing LNCaP human prostate tumor. J Nucl Med 44 (2003), 610–617.
82. [82] Nargund, V, Al Hashmi, D, Kumar, P, Gordon, S, Otitie, U, Ellison, D, et al. Imaging with radiolabelled monoclonal antibody (MUJ591) to prostate-specific membrane antigen in staging of clinically localized prostatic carcinoma: comparison with clinical, surgical and histological staging. BJU Int 95 (2005), 1232–1236.
83. 177Lu-labeled J591 antibodies specific for prostate-specific membrane antigen. J Nucl Med 46 (2005), 850–858.
84. 177Lu-labeled J591 monoclonal antibodies: effect of multiple treatments on myelotoxicity. Clin Cancer Res 11 (2005), 7195 s–7200 s.
85. 177Lu?. J Nucl Med 46 (2005), 634–641.
86. 177Lu-DOTAhuJ591 anti prostate specific membrane antigen specific monoclonal antibody. Curr Radiopharm 9 (2015), 44–53.
87. [87] Ghosh, A, Wang, X, Klein, E, Heston, WD, Novel role of prostate-specific membrane antigen in suppressing prostate cancer invasiveness. Cancer Res 65 (2005), 727–731.
88. [88] Bařinka, C, Rojas, C, Slusher, B, Pomper, M, Glutamate carboxypeptidase II in diagnosis and treatment of neurologic disorders and prostate cancer. Curr Med Chem 19 (2012), 856–870.
89. [89] Mesters, JR, Barinka, C, Li, W, Tsukamoto, T, Majer, P, Slusher, BS, et al. Structure of glutamate carboxypeptidase II, a drug target in neuronal damage and prostate cancer. EMBO J 25 (2006), 1375–1384.
90. [90] EMD Millipore, An introduction to inhibitors and their biological applications. Available at: http://www.komabiotech.co.kr/www/techniques/pdf/PB3375EN00_EM.pdf.
91. [91] Cheng, Y, Prusoff, WH, Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol 22 (1973), 3099–3108.
92. [92] Maggi, M, Filippi, S, Ledda, F, Magini, A, Forti, G, Erectile dysfunction: from biochemical pharmacology to advances in medical therapy. Eur J Endocrinol 143 (2000), 143–154.
93. [93] McGuire, JJ, Anticancer antifolates: current status and future directions. Curr Pharm Des 9 (2003), 2593–2613.
94. [94] Neale, JH, Bzdega, T, N-Acetylaspartylglutamate: the most abundant peptide neurotransmitter in the mammalian central nervous system. J Neurochem 75 (2000), 443–452.
95. [95] Olszewski, RT, Bukhari, N, Zhou, J, Kozikowski, AP, Wroblewski, JT, Shamimi-Noori, S, et al. NAAG peptidase inhibition reduces locomotor activity and some stereotypes in the PCP model of schizophrenia via group II mGluR. J Neurochem 89 (2004), 876–885.
96. [96] Subasinghe, N, Schulte, M, Chan, MY, Roon, RJ, Koerner, JF, Johnson, RL, Synthesis of acyclic and dehydroaspartic acid analogues of Ac-asp-Glu-OH and their inhibition of rat brain N-acetylated alpha-linked acidic dipeptidase (NAALA dipeptidase). J Med Chem 33 (1990), 2734–2744.
97. [97] Jackson, PF, Cole, DC, Slusher, BS, Stetz, SL, Ross, LE, Donzanti, BA, et al. Design, synthesis, and biological activity of a potent inhibitor of the neuropeptidase N-acetylated alphalinked acidic dipeptidase. J Med Chem 39 (1996), 619–622.
98. [98] Tiffany, CW, Cai, NS, Rojas, C, Slusher, BS, Binding of the glutamate carboxypeptidase II (NAALADase) inhibitor 2-PMPA to rat brain membranes. Eur J Pharmacol 427 (2001), 91–96.
99. [99] Jackson, PF, Tays, KL, Maclin, KM, Ko, YS, Li, W, Vitharana, D, et al. Design and pharmacological activity of phosphinic acid based NAALADase inhibitors. J Med Chem 44 (2001), 4170–4175.
100. [100] Wone, DW, Rowley, JA, Garofalo, AW, Berkman, CE, Optimizing phenylethylphosphonamidates for the inhibition of prostate-specific membrane antigen. Bioorg Med Chem 14 (2006), 67–76.
101. [101] Ding, P, Helquist, P, Miller, MJ, Design, synthesis and pharmacological activity of novel enantiomerically pure phosphonic acid-based NAALADase inhibitors. Org Biomol Chem 5 (2007), 826–831.
102. [102] Majer, P, Jackson, PF, Delahanty, G, Grella, BS, Ko, YS, Li, W, et al. Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor. J Med Chem 46 (2003), 1989–1996.
103. [103] Stoermer, D, Liu, Q, Hall, MR, Flanary, JM, Thomas, AG, Rojas, C, et al. Synthesis and biological evaluation of hydroxamate-based inhibitors of glutamate carboxypeptidase II. Bioorg Med Chem Lett 13 (2003), 2097–2100.
104. [104] Blank, BR, Alayoglu, P, Engen, W, Choi, JK, Berkman, CE, Anderson, MO, N-substituted Glutamyl sulfonamides as inhibitors of glutamate carboxypeptidase II (GCP2). Chem Biol Drug Des 77 (2011), 241–247.
105. [105] Majer, P, Hin, B, Stoermer, D, Adams, J, Xu, W, Duvall, BR, et al. Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1′ side chain. J Med Chem 49 (2006), 2876–2885.
106. [106] Kozikowski, AP, Nan, F, Conti, P, Zhang, J, Ramadan, E, Bzdega, T, et al. Design of remarkably simple, yet potent urea-based inhibitors of glutamate carboxypeptidase II (NAALADase). J Med Chem 44 (2001), 298–301.
107. [107] Kozikowski, AP, Zhang, J, Nan, F, Synthesis of urea-based inhibitors as active site probes of glutamate carboxypeptidase II: efficacy as analgesic agents. J Med Chem 47 (2004), 729–1738.
108. [108] Foss, CA, Mease, RC, Fan, H, Wang, Y, Ravert, HT, Dannals, RF, et al. Radiolabeled small-molecule ligands for prostate-specific membrane antigen: in vivo imaging in experimental models of prostate cancer. Clin Cancer Res 11 (2005), 4022–4028.
109. [109] Pillai, MRA, Gupte, JH, Jyotsna, T, Mani, RS, Preparation of radioiodinated insulin and thyroid stimulating hormone using 1,3,4,6-tetra chloro3α,6αdiphenyl glycouril (iodogen) for radioimmunoassay. J Radioanal Nucl Chem Articles 116 (1987), 193–202.
110. [110] Chen, Y, Foss, CA, Byun, Y, Nimmagadda, S, Pullambhatla, M, Fox, JJ, et al. Radiohalogenated prostate-specific membrane antigen (PMSA)-based ureas as imaging agents for prostate cancer. J Med Chem 51 (2008), 7933–7943.
111. [111] Wang, H, Byun, Y, Barinka, C, Pullambhatla, M, Bhang, HE, Fox, JJ, et al. Bioisosterism of urea-based GCPII inhibitors: synthesis and structure–activity relationship studies. Bioorg Med Chem Lett 20 (2010), 392–397.
112. [112] Bodei, L, Kassis, AI, Adelstein, SJ, Mariani, G, Radionuclide therapy with iodine-125 and other auger-electron-emitting radionuclides: experimental models and clinical applications. Cancer Biother Radiopharm 18 (2003), 861–877.
113. [113] Kiess, AP, Il Minn, I, Chen, Y, Hobbs, R, Sgouros, G, Mease, RC, et al. Auger radiopharmaceutical therapy targeting prostate-specific membrane antigen. J Nucl Med 56 (2015), 1401–1407.
114. [114] Maresca, KP, Hillier, SM, Femia, FJ, Keith, D, Barone, C, Joyal, JL, et al. A series of halogenated heterodimeric inhibitors of prostate specific membrane antigen (PSMA) as radiolabeled probes for targeting prostate cancer. J Med Chem 52 (2009), 347–357.
115. [115] Hillier, SM, Maresca, KP, Femia, FJ, Marquis, JC, Foss, CA, Nguyen, N, et al. Preclinical evaluation of novel glutamate-urea-lysine analogues that target prostate-specific membrane antigen as molecular imaging pharmaceuticals for prostate cancer. Cancer Res 69 (2009), 6932–6940.
116. 123I-MIP-1072, a small-molecule inhibitor of prostate-specific membrane antigen, is effective at monitoring tumor response to taxane therapy. J Nucl Med 52 (2011), 1087–1093.
117. [117] Barrett, JA, Coleman, RE, Goldsmith, ST, Vallabhajosula, S, Petry, NA, Cho, S, et al. First-in-man evaluation of two high affinity PMSA-avid small molecules for imaging prostate cancer. J Nucl Med 54 (2013), 380–387.
118. [118] Darwish, A, Blacker, M, Janzen, N, Rathmann, SM, Czorny, S, Hillier, SM, et al. Triazole appending agent (TAAG): a new synthon for preparing iodine-based molecular imaging and radiotherapy agents. ACS Med Chem Lett 8:3 (2012), 313–316.
119. [119] El-Zaria, ME, Genady, AR, Janzen, N, Petlura, CI, Beckford Vera, DR, Valliant, JF, Preparation and evaluation of carborane-derived inhibitors of prostate specific membrane antigen (PSMA). Dalton Trans 43 (2014), 4950–4961.
120. 131I-labeled small molecule (MIP-1095) targeting PSMA for prostate cancer therapy. Eur J Nucl Med Mol Imaging 41 (2014), 1280–1292.
121. 18F]FDG for use in oncology and neurosciences. Nucl Med Biol 37 (2010), 727–740.
122. 18F-DCFBC PET/CT for PSMA-based detection and characterization of primary prostate cancer. J Nucl Med 56 (2015), 1003–1010.
123. 18F-DCFPyl for prostate-specific membrane antigen antigen (PSMA)-targeted PET imaging of prostate cancer. Mol Imaging Biol 17 (2015), 565–574.
124. 18F PET/CT. Clin Genitourin Cancer 14 (2016), 115–118.
125. 18F]DCFBC: a new imaging probe for prostate cancer. Clin Cancer Res 14 (2008), 3036–3043.
126. 18F-DCFBC, a low molecular weight inhibitor of prostate-specific membrane antigen, in patients with metastatic prostate cancer. J Nucl Med 53 (2012), 1883–1891.
127. 18F-DCFBC PET/CT to conventional imaging modalities for detection of hormone-naïve and castration-resistant metastatic prostate cancer. J Nucl Med 57 (2016), 46–53.
128. 18F-DCPyl, a PSMA-based PET imaging agent for prostate cancer. Clin Cancer Res 17 (2011), 7645–7653.
129. 18F]DCFPyL via direct radiofluorination and validation in preclinical prostate cancer models. EurJ Nucl Med Mol Imaging, 6, 2016, 40, 10.1186/s13550-016-0195-6.
130. 18F-labeled phosphoramide peptidomimetic as a new prostate-specific membrane antigen-targeted imaging for prostate cancer. J Nucl Med 50 (2009), 2042–2048.
131. 18F-Glu-urea-Lys, a prostate-specific membrane antigen-based imaging agent for prostate cancer. Oncol Lett 10 (2015), 2299–2302.
132. 18F]FPy-DUPA-pep). Appl Radiat Isot 69 (2011), 1014–1018.
133. 18F(2+) chelation and biological evaluations in vitro. Mol Imaging Biol 17 (2015), 777–785.
134. [134] Ley, CR, Beattie, NR, Dannoon, S, Regan, M, VanBrocklin, H, Berkman, CE, Synthesis and evaluation of constrained phosphoramidate inhibitors of prostate-specific membrane antigen. Bioorg Med Chem Lett 25 (2015), 2536–2539.
135. 18F-labelled inhibitor of prostate-specific membrane antigen for PET imaging of prostate cancer. Eur J Nucl Med Mol Imaging 41 (2014), 89–101.
136. [136] Pomper, MG, Mease, RC, Chen, Y, Inventor: WO 2010/014933 A2. PSMA binding agents and users thereof. 2010.
137. 18F-Labeling of aromatic and heteroaromatic molecules with unprotected carboxylic acid groups. 2015.
138. [138] Banerjee, S, Pillai, MRA, Ramamoorthy, N, Evolution of Tc-99m in diagnostic radiopharmaceuticals. Sem Nucl Med 31 (2001), 260–277.
139. [139] Pillai, MRA, Dash, A, Knapp, FF Jr., Sustained availability of technetium-99m-possible paths forward. J Nucl Med 54 (2013), 313–323.
140. [140] Benesova, M, Bauder-Wüst, U, Schäfer, M, Klika, KD, Mier, W, Haberkorn, U, et al. Properties of DOTA-conjugated PSMA inhibitors. J Med Chem 59 (2016), 1761–1775.
141. 99mTc preloading strategy. J Nucl Med 48 (2007), 1379–1389.
142. [142] Banerjee, SR, Foss, CA, Castanares, M, Mease, RC, Byun, Y, Fox, JJ, et al. Synthesis and evaluation of technetium-99m- and rhenium-labeled inhibitors of the prostate-specific membrane antigen (PSMA). J Med Chem 51 (2008), 4504–4517.
143. 99mTc-radioimaging agents. Mol Pharm 6 (2009), 790–800.
144. [144] Nedrow-Byers, JR, Jabbes, M, Jewett, C, Ganguly, T, He, H, Liu, T, et al. A phosphoramidate-based prostate-specific membrane antigen-targeted SPECT agent. Prostate 72 (2012), 904–912.
145. 99mTc-labeled small molecule inhibitors of prostate-specific membrane antigen for molecular imaging of prostate cancer. J Nucl Med 54 (2013), 1369–1376.
146. 3. Appl Radiat Isot 50 (1999), 723–732.
147. [147] Nedrow-Byers, JR, Moore, AL, Ganguly, T, Hopkins, MR, Fulton, MD, Benny, PD, et al. PSMA-targeted SPECT agents: mode of binding effect on in vitro performance. Prostate 73 (2013), 355–362.
148. [148] Banerjee, SR, Pullambhatla, M, Shallai, H, Lisok, A, Mease, RC, Pomper, MG, A modular strategy to prepare multivalent inhibitors of prostate-specific membrane antigen. Oncotarget 2 (2011), 1244–1253.
149. 99mTc-labeled imaging agents for the prostate-specific membrane antigen (PSMA). J Med Chem 569 (2013), 6108–6112.
150. [150] Lowe, PS, Kularatne, SA, PSMA binding ligand-linker conjugates and methods for using. US patent 8907058 B2, 2014.
151. [151] Maresca, KP, Hillier, SM, Femia, FJ, Zimmerman, CN, Levadala, MK, Banerjee, SR, et al. Comprehensive radiolabeling, stability, and tissue distribution studies of technetium-99m single amino acid chelates (SAAC). Bioconjug Chem 20 (2009), 1625–1633.
152. mTc/Re-labeled small molecule prostate specific membrane antigen inhibitors with novel polar chelates. Bioorg Med Chem Lett 23 (2013), 1557–1563.
153. 99mTc-labeled small-molecule inhibitors of prostate-specific membrane antigen: pharmacokinetics and biodistribution studies in healthy subjects and patients with metastatic prostate cancer. J Nucl Med 55 (2014), 1791–1798.
154. [154] Maresca, K, Wang, JC, Hillier, S, Femia, F, Lu, G, Zimmermann, C, et al. Development of a simple kit for Tc-99m-MIP-1404, a single amino acid chelate (SAAC II) derived small molecule inhibitor of prostate specific membrane antigen (PSMA) for imaging prostate cancer. J Nucl Med, 53, 2012, 523 [Suppl].
155. 188W., 2010, 11–30 [IAEA Radioisotopes and Radiopharmaceuticals Series no.2].
156. [156] Knapp, FF Jr., Pillai, MRA, Osso, JA Jr., Dash, A, Re-emergence of the important role of radionuclide generators to provide diagnostic and therapeutic radionuclides to meet future research and clinical demands. J Radioanal Nucl Chem 302 (2014), 1053–1068.
157. [157] Prata, MIM, Gallium-68: a new trend in PET radiopharmacy. Curr Radiopharm 5 (2012), 142–149.
158. [158] Roesch, F, Maturation of a key resource — the germanium-68/gallium-68 generator: development and new insights. Curr Radiopharm 5 (2012), 202–211.
159. [159] Naswa, N, Sharma, P, Kumar, A, Nazar, AH, Kumar, R, Chumber, S, et al. Gallium-68-DOTA-NOC PET/CT of patients with gastroenteropancreatic neuroendocrine tumors: a prospective single-center study. AJR Am J Roentgenol 97 (2011), 1221–1228.
160. [160] Bodei, L, Mueller-Brand, J, Baum, RP, Pavel, ME, Hörsch, D, O'Dorisio, MS, et al. The joint IAEA, EANM, and SNMMI practical guidance on peptide receptor radionuclide therapy (PRRNT) in neuroendocrine tumours. Eur J Nucl Med Mol Imag 40 (2013), 800–816.
161. [161] Kubícek, V, Havlícková, J, Kotek, J, Tircsó, G, Hermann, P, Tóth, E, et al. Gallium(III) complexes of DOTA and DOTA-monoamide: kinetic and thermodynamic studies. Inorg Chem 49 (2010), 10960–10969.
162. 68Ga-labeled inhibitors of prostate-specific membrane antigen (PSMA) for imaging prostate cancer. J Med Chem 53 (2010), 5333–5341.
163. 68Ga-complex lipophilicity and the targeting property of a urea-based PMSA inhibitor for PET imaging. Bioconj Chem 23 (2012), 688–697.
164. [164] Martell, AE, Motekaitis, RJ, Clarke, ET, Harisson, JJ, Synthesis of N,N′-di(2-hydroxybenzyl)ethylenediamine,N-N′-diacetic acid (HBED) and derivatives. Can J Chem 64 (1986), 449–456.
165. [165] Pillai, MRA, Lo, JM, John, CS, Schlemper, EO, Troutner, DE, μ-Oxo-bis-oxo complexes of Tc(V) with amine phenol ligands: synthesis, characterization, and X-ray crystal structures. Inorg Chem 29 (1990), 1850–1856.
166. [166] Pillai, MRA, Barnes, CL, Schlemper, EO, Dinuclear complexes of Re(V) with amine-phenol ligands. Syntheses, characterization and X-ray crystal structures. Polyhedron 13 (1994), 701–708.
167. [167] Pillai, MRA, Barnes, CL, Schlemper, EO, Dinuclear complexes of rhodium (III) with an amine-phenol ligand: synthesis and X-ray crystal structure. Crystal Spect Res 23 (1993), 719–723.
168. [168] Pillai, MRA, Schlemper, EO, Palladium (II) complexes of a tetradentate amine-phenol ligand. J Cryst Spect Res 24 (1994), 127–130.
169. 105Rh] rhodium using a pentadentate bifunctional ligand. Bioconj Chem 1 (1990), 191–197.
170. [170] Zöller, M, Schuhmacher, J, Reed, J, Maier-Borst, W, Matzku, S, Establishment and characterization of monoclonal antibodies against an octahedral Ga-chelate suitable for immunoscintigraphy with PET. J Nucl Med 33 (1992), 1366–1372.
171. [171] Kiess, AP, Banerjee, SR, Mease, RC, Rowe, SP, Rao, A, Foss, CA, et al. Prostate-specific membrane antigen as a target for cancer imaging and therapy. Q J Nucl Med Mol Imaging 59 (2015), 241–268.
172. 68Ga]Ga-PSMA-HBED-CC: a new PET tracer for imaging of prostate cancer. Pharmaceutics (Basel) 7 (2014), 779–796.
173. 68Ga-PET imaging of prostate cancer. Eur J Nucl Med Mol Imaging Res, 2, 2012, 23.
174. [174] Liolios, C, Schäfer, M, Haberkorn, U, Eder, M, Kopka, K, Novel bispecific PSMA/GRPr targeting Radioligands with optimized pharmacokinetics for improved PET imaging of prostate cancer. Bioconjug Chem 27 (2016), 737–751.
175. [175] Eisenwiener, KP, Powell, P, Mäcke, HR, A convenient synthesis of novel bifunctional prochelators for coupling to bioactive peptides for radiometal labelling. Bioorg Med Chem Lett 18 (2000), 2133–2135.
176. [176] Weineisen, M, Simecek, J, Schottelius, M, Schwaiger, M, Wester, HJ, Synthesis and preclinical evaluation of DOTAGA-conjugated PSMA ligands for functional imaging and endoradiotherapy of prostate cancer. Eur J Nucl Med Mol Imaging Res, 4, 2014, 63.
177. 177Lu-labeled PMSA I&T: optimization of a PMSA-targeted theranostic concept first proof-of-concept in human studies. J Nucl Med 56 (2015), 1169–1176.
178. [178] Gourni, E, Canovas, C, Goncalves, V, Denat, F, Meyer, PT, Maecke, HR, (R)-NODAGA-PSMA: a versatile precursor for radiometal Leling and nuclear imaging of PSMA-positive tumors. PLoS ONE, 10(12), 2015, e0145755, 10.1371/journal.pone.0145755.
179. [179] Baur, B, Solbach, C, Andreolli, E, Winter, G, Machulla, H-J, Reske, SN, Synthesis, radiolabelling and in vitro characterization of the gallium-68-, yttrium-90- and lutetium-177-labelled PSMA ligand, CHX-A”-DTPA-DUPA-pep. Pharmaceuticals 7 (2014), 517–529.
180. [180] Zhu, C, Bandekar, A, Sempkowski, M, Banerjee, SR, Pomper, MG, Bruchertseifer, F, et al. Nanoconjugation of PSMA-targeting ligands enhances perinuclear localization and improves efficacy of delivered alpha-particle emitters against tumor endothelial analogues. Mol Cancer Ther 15 (2016), 106–113.
181. [181] Elgqvist, J, Frost, S, Pouget, J-P, Albertsson, P, The potential and hurdles of targeted alpha therapy — clinical trials and beyond. Front Oncol, 3, 2013, 324.
182. [182] Pillai, MRA, Knapp, FF Jr., Evolving important role of lutetium-177 for therapeutic nuclear medicine. Curr Radiopharm 8 (2015), 78–85.
183. [183] Banerjee, S, Pillai, MRA, Knapp, FF Jr., Lutetium-177 therapeutic radiopharmaceuticals — linking chemistry, radiochemistry and practical applications. Chem Rev 115 (2015), 2934–2974.
184. 176Yb: options for ytterbium/lutetium separation. Curr Radiopharm 8 (2015), 107–118.
185. 177Lu for targeted radionuclide therapy: available options. Nucl Med Mol Imaging 49 (2015), 85–107.
186. [186] Luetje, S, Heskamp, S, Cornelissen, AS, Poeppel, TD, van den Broek, SA, Rosenbaum-Krumme, S, et al. PMSA ligands for radionuclide imaging and therapy of prostate cancer: clinical status. Theranos 5 (2015), 1388–1401.
187. 68Ga generator. Nucl Med Biol 43 (2016), 463–469.
188. 68Ga-DKFZ-PSMA-11 and its performance in prostate cancer patients. Molecules 20 (2015), 14860–14878.
189. 68Ga]DKFZ-PSMA-11 using a robust single-vial kit and demonstration of its clinical efficacy. Mol Imaging Biol, 16, 2016 Mar [Epub ahead of print PubMed PMID: 26983703].
190. 68Ga]gallium-labelled PSMA ligand for the diagnosis of prostate ccancer: biodistribution in humans and first evaluation of tumor lesions. Eur J Nucl Med Mol Imaging 40 (2013), 969–970.
191. [191] Afshar-Oromieh, A, Zechmann, CM, Malcher, A, Eder, M, Eisenhut, M, Linhart, HG, et al. Comparison of PET imaging with a (68)Ga-labelled PSMA ligand and (18)F-choline-based PET/CT for the diagnosis of recurrent prostate cancer. Eur J Nucl Med Mol Imaging 41 (2014), 11–20.
192. 18F-choline-PET/CT. Clin Nucl Med, 2016 [Epub ahead of print].
193. [193] Afshar-Oromieh, A, Avtzi, E, Giesel, FL, Holland-Letz, T, Linhart, HG, Eder, M, et al. Haberkorn UThe diagnostic value of PET/CT imaging with the (68)Ga-labelled PSMA ligand HBED-CC in the diagnosis of recurrent prostate cancer. Eur J Nucl Med Mol Imaging 42 (2015), 197–209, 10.1007/s00259-014-2949-6 [Epub 2014 Nov 20].
194. [194] Sterzing, F, Kratochwil, C, Fiedler, H, Katayama, S, Habl, G, Kopka, K, et al. (68)Ga-PSMA-11 PET/CT: a new technique with high potential for the radiotherapeutic management of prostate cancer patients. Eur J Nucl Med Mol Imaging 43 (2016), 34–41.
195. 68Ga(HBED-CC)] versus 3D CT volumetric lymph node assessment in recurrent prostate cancer. Eur J Nucl Med Mol Imaging 42 (2015), 1794–1800.
196. 68Ga]Ga-PSMA-HBED-CC for PSMA-PET imaging in patients with relapsed prostate cancer. Mol Imaging Biol 17 (2015), 575–584.
197. [197] Giesel, FL, Sterzing, F, Schlemmer, HP, Holland-Letz, T, Mier, W, Rius, M, et al. Intra-individual comparison of (68)Ga-PSMA-11-PET/CT and multi-parametric MR for imaging of primary prostate cancer. Eur J Nucl Med Mol Imaging 43 (2016), 1400–1406.
198. 68Ga-PSMA PET/CT in the evaluation of lymph node and bone metastases of prostate cancer. Eur J Nucl Med Mol Imaging 43 (2016), 70–83.
199. 68Ga-PSMA positron emission tomography/computed tomography provides accurate staging of lymph node regions prior to lymph node dissection in patients with prostate cancer. Eur Urol, 2016, 10.1016/j.eururo.2015.12.051 [pii: S0302–2838(16)00009–9. [Epub ahead of print] PMID: 26810345].
200. [200] Maurer, T, Weirich, G, Schottelius, M, Weineisen, M, Frisch, B, Okur, A, et al. Prostate-specific membrane antigen-radioguided surgery for metastatic lymph nodes in prostate cancer. Eur Urol 68 (2015), 530–534.
201. 68Ga-PMSA ligand PET/CT in 248 patients with biochemical recurrence after radical prostatectomy. J Nucl Med 56 (2015), 668–674.
202. [202] Evangelista, L, Fattoni, F, Rossi, E, Karnes, RJ, Lowe, V, Early detection of prostate cancer relapse by biochemistry and diagnostic imaging. Q J Nucl Med Mol Imaging 59 (2015), 359–373.
203. 68Ga-PSMA PET in patients with biochemically recurrent prostate cancer. J Nucl Med 57 (2016), 557–562.
204. 68Ga-PSMA PET/CT in prostate cancer patients who haverising PSA after curative treatment and are being considered for targeted therapy. J Nucl Med 56 (2016), 1185–1190.
205. 68Ga-PSMA-HBED-CC PET/CT: where molecular imaging has as edge over morphological imaging. Eur J Nucl Med Mol Imaging 43 (2015), 394–396.
206. 68Ga-labelled prostate-specific membrane antigen (PSMA) in the management of patient with organ confined and locally advanced prostate cancer prior to radical treatment and after radical prostatectomy. Urology, 2016, 10.1016/j.urology.2015.12.048 [pii: S0090–4295(16)00011-X. [Epub ahead of print] Review. PMID: 2679058].
207. 68Ga]PSMA-HBED-CC PET/CT in relation to PSA levels, PSA doubling time and Gleason score. Eur J Nucl Med Mol Imaging 43 (2016), 397–403.
208. 68Ga-PSMA PET/CT. Clin Nucl Med 40 (2015), 755–756.
209. 68Ga-labeled anti-prostate-specific membrane antigen peptide as marker for androgen deprivation therapy response in prostate cancer. Clin Nucl Med 41 (2016), 423–425.
210. [210] Sachpekidis, C, Eder, M, Kopka, K, Mier, W, Hadaschik, BA, Haberkorn, U, et al. (68)Ga-PSMA-11 dynamic PET/CT imaging in biochemical relapse of prostate cancer. Eur J Nucl Med Mol Imaging 43 (2016), 1288–1299.
211. 68Ga-PSMA PET/CT. Clin Nucl Med 41 (2016), 294–295.
212. 68Ga-PSMA PET/CT for restaging recurrent prostate cancer: which factors are associated with PET/CT detection rate?. Eur J Nucl Med Mol Imaging 42 (2015), 1282–1294.
213. 153Sm-EDTMP bone pain palliation therapy. Clin Nucl Med 41 (2016), 353–354.
214. [214] Radiation therapy for prostate cancer. Available from: http://www.cancer.org/cancer/prostatecancer/detailedguide/prostate-cancer-treating-radiation-therapy.
215. [215] Afshar-Oromieh, A, Hetzheim, H, Kratochwil, C, Benesova, M, Eder, M, Neels, OC, et al. The theranostic PSMA ligand PSMA-617 in the diagnosis of prostate cancer by PET/CT: biodistribution in humans, radiation dosimetry, and first evaluation of tumor lesions. J Nucl Med 56 (2015), 1697–1705.
216. [216] Hohberg, M, Eschner, W, Schmidt, M, Dietlein, M, Kobe, C, Fischer, T, et al. Lacrimal glands may represent organs at risk for radionuclide therapy of prostate cancer with [(177)Lu]DKFZ-PSMA-617. Mol Imaging Biol 18 (2016), 437–445.
217. [217] Delker, A, Fendler, WP, Kratochwil, C, Brunegraf, A, Gosewisch, A, Gildehaus, FJ, et al. Dosimetry for (177)Lu-DKFZ-PSMA-617: a new radiopharmaceutical for the treatment of metastatic prostate cancer. Eur J Nucl Med Mol Imaging 43 (2016), 42–51.
218. [218] Kratochwil, C, Giesel, FL, Stefanova, M, Benešová, M, Bronzel, M, Afshar-Oromieh, A, et al. PSMA-targeted radionuclide therapy of metastatic castration-resistant prostate cancer with Lu-177 labeled PSMA-617. J Nucl Med, 2016 [pii: numed.115.171397. [Epub ahead of print] PubMed PMID].
219. 177Lu-DKFZ-617 PSMA of castrate-resistant metastatic prostate cancer: a two Centre study. Eur J Nucl Med Med Imaging, 5, 2015, 114.
220. 177Lu-PSMA-DKFZ-617 of castrate-resistant metastatic prostate cancer. Oncotarget 7 (2016), 12477–12488.
221. 177Lu PSMA-617 therapy on bone marrow depression caused by metastatic prostate cancer. Clin Nucl Med 41 (2016), 478–480.
222. 177Lu-PSMA-617. Clin Nucl Med 41 (2016), 572–573.
223. 177Lu-labeled PSMA-617: initial experience in prostate cancer patients. Nucl Med Biol 43 (2016), 296–302.
224. 177Lu prostate-specific membrane antigen treatment in patient with metastatic prostate cancer. Clin Nucl Med 41 (2016), 159–160.
225. 177Lu-labeled PSMA inhibitor. J Label Compd Radiopharm, 2016, 10.1002/jlcr.3414 [ wileyonlinelibrary.com].
226. [226] Kabasakal, L, AbuQbeitah, M, Aygün, A, Yeyin, N, Ocak, M, Demirci, E, et al. Pre-therapeutic dosimetry of normal organs and tissues of (177)Lu-PSMA-617 prostate-specific membrane antigen (PSMA) inhibitor in patients with castration-resistant prostate cancer. Eur J Nucl Med Mol Imaging 42 (2015), 1976–1983.
227. 177Lu-labeled PSMA I&T: optimization of a PSMA-targeted theranostic concept and first proof-of-concept human studies. J Nucl Med 56 (2015), 1169–1176.
228. [228] Advanced accelerator applications signs exclusive license agreement with Johns Hopkins University to develop PSMA receptor ligand in prostate cancer. Available from: https://globenewswire.com/news-release/2016/01/11/800819/0/en/Advanced-Accelerator-Applications-Signs-Exclusive-License-Agreement-With-Johns-Hopkins-University-to-Develop-PSMA-Receptor-Ligand-in-Prostate-Cancer.html.
229. [229] Progenics pharmaceuticals presents PSMA-related data at SNMMI 2013. Findings support potential role of prostate specific membrane antigen in targeted imaging and therapy. http://ir.progenics.com/releasedetail.cfm?releaseid=770303.
230. [230] Ristau, BT, O'Keefe, DS, Babich, DJ, The prostate-specific membrane antigen: lessons and current clinical implications from 20 years of research. Urol Oncol 32 (2014), 272–279.
231. [231] Samplaski, MK, Heston, W, Elson, P, Magi-Galluzzi, C, Hansel, DE, Folate hydrolase (prostate-specific membrane [corrected] antigen) 1 expression in bladder cancer subtypes and associated tumor neovasculature. Mod Pathol 11 (2011), 1521–1529.
232. 68Ga-PSMA imaging of metastatic breast cancer. Eur J Nucl Med Mol Imaging 42 (2015), 1482–1483.
233. 68Ga] PSMA-HBED pet for differential diagnosis of suspicious lung lesions in patients with prostate cancer. J Nucl Med 57 (2015), 367–371.
234. 68Ga prostate-specific membrane antigen activity in metastatic non-small cell lung cancer. Clin Nucl Med 41 (2016), 414–416.
235. 68Ga]PSMA-HBED-CC PET/CT. Eur J Nucl Med Mol Imaging 42 (2015), 1622–1623.
236. 68Ga-PSMA PET/CT imaging in primary hepatocellular carcinoma. Eur J Nucl Med Mol Imaging 43 (2016), 795–796.
237. 18F-DCFPyL. Ann Nucl Med 29 (2015), 877–882.
238. [238] Schwenck, J, Tabatabai, G, Skardelly, M, Reischl, G, Beschorner, R, Pichler, B, et al. In vivo visualization of prostate-specific membrane antigen in glioblastoma. Eur J Nucl Med Mol Imaging 42 (2015), 170–171.
239. 68Ga-PSMA PET/CT in a paravertebral schwannoma mimicking prostate cancer metastasis. Eur J Nucl Med Mol Imaging 43 (2016), 193–194.
240. [240] Sasikumar, A, Joy, A, Pillai, MRA, Nanabala, R, Hari, TA, Ga-68 PSMA PET/CT-false positive tracer uptake in Paget's disease. Clin Nucl Med, 2016 [in press].
241. 18F-DCFPyL in Paget's disease of bone, an important potential pitfall in clinical interpretation of PSMA PET studies. Tomography 1 (2015), 81–84.
242. [242] Chaux, A, Eifler, J, Karram, S, Al-Hussain, T, Faraj, S, Pomper, M, et al. Focal positive prostate-specific membrane antigen (PSMA) expression in ganglionic tissues associated with prostate neurovascular bundle: implications for novel intraoperative PSMA-based fluorescent imaging techniques. Urol Oncol 31 (2013), 572–575.
243. 68Ga]PSMA-HBED uptake mimicking lymph node metastasis in coeliac ganglia: an important pitfall in clinical practice. Eur J Nucl Med Mol Imaging 42 (2015), 210–214.
244. [244] Pillai, MRA, Das, T, Options to meet the future global demand of radionuclides for radionuclide therapy. Nucl Med Biol 40 (2013), 23–32.
245. [245] Chakravarty, R, Dash, A, Pillai, MRA, Availability of yttrium-90 from strontium-90: a nuclear medicine perspective. Cancer Biother Radiopharm 27 (2012), 621–641.
246. 90Y]DOTA-DUPA-pep for clinical applications. J Nucl Med, 55, 2014, 1149 [Suppl].
247. [247] Wustemann, T, Bauder-Wust, U, Schafer, M, Eder, M, Benesova, M, Leotta, K, et al. Design of internalizing PSMA-specific Glu-urea-based radiotherapeutics. Theranostics 6 (2016), 1085–1095.
248. 177Lu-PSMA is set to redefine prostate cancer treatment. Curr Radiopharm 9 (2016), 6–7.